Abstract:
A method for selectively inhibiting a kinase is disclosed, which comprises contacting a composition containing a kinase with a molecule of formula (I) wherein R1 is H, lower alkyl, or lower alkanoyl; R2 is H, lower alkyl, or lower alkanoyl; R3 and R4 together represent a cis double bond or -O- or each of R3 and R4 independently represents H or OR; R5 is =O, =S, or -H, -OR; R6 and R7 together represent a double bond or -O- or each of R6 and R7 independently represents H or OR; R8 and R9 together represent a double bond or -O- or each of R8 and R9 independently represents H or OR; and each R independently represents H, lower alkyl, or lower alkanoyl.
Abstract:
The DNA encoding the C140 cell surface receptor has been cloned and sequenced. The availability of this DNA permits the recombinant production of the C140 receptor which can be produced at cell or oocyte surfaces and is useful in assay systems both for the detection of substances which affect its activity, including agonists and antagonists. Further, the elucidation of the structure of the C140 receptor permits the design of agonist and antagonist compounds which are useful in these assays. The availability of the C140 receptor also permits production of antibodies specifically immunoreactive with the receptor per se or with specific regions thereof.
Abstract:
Reagents that specifically bind a carbohydrate target wherein sialic acid is linked at the nonreducing terminus of a glycoside to a galactose or galactosamine residue through an alpha 2-6 linkage are able to inhibit the conversion of human Factor X to human Factor Xa. These reagents (SA/Gal/GalNAc binding reagents) as well as other strategies for inhibiting the conversion of Factor X to Factor Xa are useful in treating thrombosis, inflammation and other conditions associated with excess thrombin activity.
Abstract translation:特异性结合碳水化合物靶标的试剂能够抑制人因子X向人因子Xa的转化,其中唾液酸在糖苷的非还原性末端通过α2-6键连接到半乳糖或半乳糖胺残基。 这些试剂(SA / Gal / GalNAc结合试剂)以及抑制因子X转化成因子Xa的其它策略可用于治疗血栓形成,炎症和与过量凝血酶活性相关的其它病症。
Abstract:
Platelet antiadhesives (PAA) which are useful as antithrombotics are obtainable from snake venoms which have been identified using an assay which measures the ability of the venom to inhibit ristocetin- or botrocetin-induced agglutination of platelets in the presence of von Willebrand Factor. The antiadhesives of the invention are 20-24 kd dimers of smaller peptides, or effective portions thereof. Antibodies to these antiadhesives are also prepared and are useful in assays for PAA and for screening expression libraries for PAA encoding DNA.
Abstract:
An assay for screening snake venom for the presence or absence of platelet aggregation inhibitors (PAIs) based on specific receptor binding is described. Using this assay, the identification and characterization of PAIs in a wide range of snake venom samples was accomplished. The isolated and purified PAI from several of these active snake venoms is described and characterized. In addition, PAIs lacking the Arg-Gly-Asp (RGD) adhesion sequence but containing K* -(G/Sar)-D wherein K* is a modified lysyl residue of the formula R 2 N(CH2)4CHNHCO- wherein each R is independently H, alkyl(1-6C) or at most one R is R -C=NR wherein R is H, alkyl(1-6C), phenyl or benzyl, or is NR in which each R is independently H or alkyl(1-6C) and R is H, alkyl(1-6C), phenyl or benzyl, or R -C=NR is a radical selected from the group consisting of (a), (b), (c) and (d) where m is an integer of 2-3, and each R is independently H or alkyl(1-6C); and wherein one or two (CH2) may be replaced by O or S provided said O or S is not adjacent to another heteroatom are prepared and shown to specifically inhibit the binding of fibrinogen or von Willebrand Factor to GP IIb-IIIa.
Abstract:
Analogs of blood factors which are transiently inactive are useful in treatment of diseases characterized by thrombosis. In addition, modified forms of activated blood factors that generate the active blood factor in serum but have extended half-lives are useful in treating hemophilic conditions. These modified forms of the blood factor may be acylated forms which are slowly deacylated in vivo.
Abstract:
The present invention is directed towards immunoglobulin polypeptides that specifically bind to the extracellular domain of the human type beta PDGF receptor. The binding of the immunoglobulin polypeptides to the receptor inhibits PDGF-induced (or stimulated) receptor activation as indicated by inhibition of receptor phosphorylation and dimerization, and by inhibition of PDGF-mediated mitogenesis, chemotaxis and migration of cells displaying the human PDGF type beta receptor on the cell surface. Nucleic acids encoding the immunoglobulin polypeptides are also included in the invention. The immunoglobulin polypeptides have diagnostic and therapeutic uses.
Abstract:
This invention relates to the glycoprotein v gene. Specifically, this invention discloses the sequence and structure of the glycoprotein v gene and the amino acid sequence of the glycoprotein v polypeptide. In addition, the evolutionary relationship of the glycoprotein v gene with other glycoproteins is described and several uses of the isolated glycoprotein v gene are shown.
Abstract:
The present invention provides the amino acid and nucleotide sequence of a protein that binds to null3 integrins, nullIIb and Src kinase and is involved in integrin mediated signaling. Based on this disclosure, the present invention provides methods for identifying agents that block integrin mediated signaling, methods of using agents that block integrin mediated signaling to modulate biological and pathological processes, and agents that block integrin mediated signaling
Abstract:
Systems, devices, and methods are provided for removing carbon dioxide from a target fluid, such as, for example, blood, to treat hypercarbic respiratory failure or another condition. A device is provided including first and second membrane components for removing dissolved gaseous carbon dioxide and bicarbonate from the fluid, which can be done simultaneously. The device can be in the form of a cartridge configured for use in a dialysis system. A method of treatment is also provided, involving drawing blood from a patient and bringing the patient's blood in contact with a first membrane component having a sweep gas passing therethrough, and a second membrane component having a dialysate passing therethrough. The dialysate's composition can be selected such that charge neutrality is maintained.